CA3058448A1 - Piperidines as covalent menin inhibitors - Google Patents

Piperidines as covalent menin inhibitors Download PDF

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Publication number
CA3058448A1
CA3058448A1 CA3058448A CA3058448A CA3058448A1 CA 3058448 A1 CA3058448 A1 CA 3058448A1 CA 3058448 A CA3058448 A CA 3058448A CA 3058448 A CA3058448 A CA 3058448A CA 3058448 A1 CA3058448 A1 CA 3058448A1
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CA
Canada
Prior art keywords
group
compound
pharmaceutically acceptable
solvate
acceptable salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3058448A
Other languages
English (en)
French (fr)
Inventor
Shaomeng Wang
Angelo AGUILAR
Shilin Xu
Liyue HUANG
Jeanne STUCKEY
Xu TIANFENG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Michigan System
Original Assignee
University of Michigan System
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by University of Michigan System filed Critical University of Michigan System
Publication of CA3058448A1 publication Critical patent/CA3058448A1/en
Pending legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
CA3058448A 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors Pending CA3058448A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762479520P 2017-03-31 2017-03-31
US62/479,520 2017-03-31
PCT/US2018/025417 WO2018183857A1 (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Publications (1)

Publication Number Publication Date
CA3058448A1 true CA3058448A1 (en) 2018-10-04

Family

ID=63677047

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3058448A Pending CA3058448A1 (en) 2017-03-31 2018-03-30 Piperidines as covalent menin inhibitors

Country Status (14)

Country Link
US (1) US11045448B2 (enrdf_load_stackoverflow)
EP (1) EP3600313A4 (enrdf_load_stackoverflow)
JP (1) JP2020515571A (enrdf_load_stackoverflow)
KR (1) KR20190133224A (enrdf_load_stackoverflow)
CN (1) CN110636843A (enrdf_load_stackoverflow)
AU (1) AU2018243586A1 (enrdf_load_stackoverflow)
BR (1) BR112019020130A2 (enrdf_load_stackoverflow)
CA (1) CA3058448A1 (enrdf_load_stackoverflow)
EA (1) EA201992320A1 (enrdf_load_stackoverflow)
IL (1) IL269542A (enrdf_load_stackoverflow)
MX (1) MX2019011412A (enrdf_load_stackoverflow)
PH (1) PH12019502263A1 (enrdf_load_stackoverflow)
SG (1) SG11201909083UA (enrdf_load_stackoverflow)
WO (1) WO2018183857A1 (enrdf_load_stackoverflow)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017192543A1 (en) 2016-05-02 2017-11-09 Regents Of The University Of Michigan Piperidines as menin inhibitors
EP3774731A4 (en) * 2018-03-30 2021-11-24 The Regents Of The University Of Michigan PIPERIDINE COMPOUNDS AS COVALENT MENINE INHIBITORS
CA3112340A1 (en) 2018-10-03 2020-04-09 The Regents Of The University Of Michigan Small molecule menin inhibitors
KR102726437B1 (ko) 2018-12-31 2024-11-05 바이오메아 퓨전, 인크. 메닌-mll 상호작용의 비가역적 억제제
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
TW202126636A (zh) 2019-09-30 2021-07-16 美商阿吉歐斯製藥公司 作為ｍｅｎｉｎ抑制劑之六氫吡啶化合物
TW202204333A (zh) 2020-04-08 2022-02-01 美商阿吉歐斯製藥公司 Menin抑制劑及治療癌症之使用方法
WO2021207310A1 (en) 2020-04-08 2021-10-14 Agios Pharmaceuticals, Inc. Menin inhibitors and methods of use for treating cancer
CA3202151A1 (en) * 2020-12-16 2022-06-23 Biomea Fusion, Inc. Fused pyrimidine compounds as inhibitors of menin-mll interaction
AU2022325861A1 (en) 2021-08-11 2024-02-29 Biomea Fusion, Inc. Covalent inhibitors of menin-mll interaction for diabetes mellitus
US12018032B2 (en) 2021-08-20 2024-06-25 Biomea Fusion, Inc. Crystalline forms of N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide as an irreversible inhibitor of menin-MLL interaction
WO2023056589A1 (en) 2021-10-08 2023-04-13 Servier Pharmaceuticals Llc Menin inhibitors and methods of use for treating cancer
CN120529900A (zh) 2022-11-24 2025-08-22 奥莱松基因组股份有限公司 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合
WO2024155710A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6- yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2-pyridinecarboxamide as a covalent inhibitor of menin-mll interaction

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JP5792171B2 (ja) 2009-09-04 2015-10-07 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 白血病を治療するための組成物および方法
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KR102726437B1 (ko) 2018-12-31 2024-11-05 바이오메아 퓨전, 인크. 메닌-mll 상호작용의 비가역적 억제제
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction

Also Published As

Publication number Publication date
CN110636843A (zh) 2019-12-31
MX2019011412A (es) 2020-02-07
IL269542A (en) 2019-11-28
BR112019020130A2 (pt) 2020-04-22
SG11201909083UA (en) 2019-10-30
AU2018243586A1 (en) 2019-10-17
EA201992320A1 (ru) 2020-04-22
KR20190133224A (ko) 2019-12-02
JP2020515571A (ja) 2020-05-28
US20200022953A1 (en) 2020-01-23
WO2018183857A1 (en) 2018-10-04
US11045448B2 (en) 2021-06-29
EP3600313A1 (en) 2020-02-05
PH12019502263A1 (en) 2020-10-26
EP3600313A4 (en) 2020-09-23

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